Sustained release pharmaceutical compositions for the parenteral administration of hydrophilic compounds

a technology of hydrophilic compounds and pharmaceutical compositions, which is applied in the direction of drug compositions, somatostatins, peptides, etc., can solve the problems of conversely unacceptable intolerantness in the form of persistent ulcerations, and achieve the effect of sustained release of hydrophilic active ingredients

Inactive Publication Date: 2007-01-02
ITALFARMACO SPA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0019]The present invention aims at providing sustained release pharmaceutical compositions in the form of stable w / o microemulsions, which are easy to prepare, can be sterilized, are free from remarkable systemic or topical side effects, are suitable for parenterally administering, preferably i.m. or s.c., active ingredients which are hydrophilic or are made hydrophilic through suitable derivatization, thereby obtaining a remarkable technical improvement compared with the known technique.

Problems solved by technology

A local intolerance in the form of persistent ulcerations is conversely considered unacceptable.

Method used

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  • Sustained release pharmaceutical compositions for the parenteral administration of hydrophilic compounds
  • Sustained release pharmaceutical compositions for the parenteral administration of hydrophilic compounds
  • Sustained release pharmaceutical compositions for the parenteral administration of hydrophilic compounds

Examples

Experimental program
Comparison scheme
Effect test

example 2

Preparation of a w / o Microemulsion Containing Leuprolide Acetate

[0045]The procedure of Example 1 is followed, but solubilizing 600 mg of Leuprolide acetate in 10 ml of water.

example 3

Preparation of a w / o Microemulsion Containing Leuprolide Acetate

[0046]The procedure of Example 1 is followed, but without adding 200 mg of lysine. Calculated pH is about 3.

example 4

Preparation of a w / o Microemulsion Containing Leuprolide Acetate

[0047]The procedure of Example 1 is followed, but solubilizing 900 mg of Leuprolide acetate in 10 ml of water.

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Abstract

Stable, biologically compatible pharmaceutical compositions in the form of water-in-oil microemulsions (w / o), for the sustained release by parenteral administration of active ingredients which are hydrophilic or are made hydrophilic by suitable derivatization, a process for the preparation of said microemulsions and the use thereof.

Description

FIELD OF THE INVENTION[0001]The present invention relates to sustained release pharmaceutical compositions for the parenteral administration of active ingredients which are hydrophilic or are made hydrophilic by suitable derivatization, in the form of stable, biologically compatible and easily preparable water-in-oil microemulsions (w / o). More particularly, peptide active ingredients or biologically active oligo- or polysaccharides, for which protection from the immediate attack by the hydrolytic enzymes present in living organisms as well as sustained release in time, to avoid repeated administrations, are desirable, are advantageously formulated through said microemulsions. Said formulations for the therapeutical use can be injected without problems or significant side effects and are easily prepared industrially, providing a remarkable technical improvement.PRIOR ART[0002]Microemulsions can be generally defined as optically isotropic systems, not birifrangent under polarized ligh...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K9/127A61K9/107A61K31/702A61K31/715A61K31/727A61K38/00A61K38/04A61K45/00A61K47/10A61K47/12A61K47/14A61K47/24A61K47/26A61K47/28A61K47/34A61P5/02A61P5/24
CPCA61K9/1075A61P35/00A61P5/02A61P5/06A61P5/24A61P5/26A61K9/107
Inventor AUTUORI, FRANCESCOBIANCHINI, CARLOBOTTONI, GIUSEPPELEONI, FLAVIOMASCAGNI, PAOLOMONZANI, VALMENPICCOLO, ORESTE
Owner ITALFARMACO SPA
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